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Aurothiomalate sodium

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Chemical Structure| 12244-57-4 同义名 : 金硫丁二酸钠
CAS号 : 12244-57-4
货号 : A429214
分子式 : C4H6AuNaO4S
纯度 : 99%+
分子量 : 370.109
MDL号 : MFCD00064304
存储条件:

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

H2O: 250 mg/mL(675.48 mM),配合低频超声助溶

动物实验配方:
生物活性
描述 Aurothiomalate sodium is a potent and selective inhibitor of oncogenic PKCι signalling. Aurothiomalate sodium inhibits tumour cell proliferation but not apoptosis. Aurothiomalate sodium is a potent inhibitor of TrxR. Aurothiomalate sodium is an antirheumatic drug with strong antitumour activity[1][2][3].At concentrations of 0.001, 0.01, 0.1, 1, 10, 100, and 1000 uM, Aurothiomalate sodium induced inhibition of anchorage-independent growth in a dose-dependent manner in subject cell lines with IC50 of 300 nM-107 µM. Aurothiomalate sodium can induce inhibition of anchorage-independent growth in a dose-dependent manner with an IC50 of 300 nM-107 µM, including the A549, H1437, H2170, H460, H510, H187, H1703, and A427 lung cancer cell lines. Lung adenocarcinoma (LAC) and small cell lung cancer (SCLC) cells were more sensitive to Aurothiomalate sodium, while lung adenocarcinoma (LAC) was less sensitive to Aurothiomalate sodium. Aurothiomalate sodium blocked PKCι-Par6- by binding PKCι Rac1-Pak-Mek 1,2-Erk 1,2 signalling pathway activation and inhibits the growth of non-small lung cancer (NSCLC)[1].Aurothiomalate sodium inhibits TNFα-induced NF-kB activation and the expression of NF-kB-targeted pro-inflammatory genes (e.g., E-selectin and COX-2) at a concentration of 25 uM for 6 hours[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.70mL

0.54mL

0.27mL

13.51mL

2.70mL

1.35mL

27.02mL

5.40mL

2.70mL

参考文献

[1]Roderick P Regala, et al. Atypical protein kinase C iota expression and aurothiomalate sensitivity in human lung cancer cells. Cancer Res. 2008 Jul 15;68(14):5888-95.

[2]Roderick P Regala, et al. Atypical protein kinase C{iota} is required for bronchioalveolar stem cell expansion and lung tumorigenesis. Cancer Res. 2009 Oct 1;69(19):7603-11.

[3]Atsuko Sakurai, et al. Overexpression of thioredoxin reductase 1 regulates NF-kappa B activation. J Cell Physiol. 2004 Jan;198(1):22-30.